D-I03

D-I03

Biochem/physiol Actions

D-I03 is a selective RAD52 inhibitor (IC50 = 5 and 8 µM, respectively, by SSA and DNA pairing (D-loop formation) assay; ﹤5% RAD51 inhibition at 80 µM) that blocks single-strand DNA (ssDNA) annealing (SSA)-, but not homology dependent recombination (HDR)-, mediated double-strand break (DSB) repair (5-30 µM using respective U2OS reporter cells) and reduces nuclear RAD52, but not RAD51, foci formation (2.5 µM) upon DNA damage by cisplatin. D-I03 selectively suppresses BRCA1-deficient over BRCA1-proficient cancer cells and exerts synergistic activity with PARP1 inhibitors against BRCA1-deficient cancer both in cultures (1 & 2.5 µM) and in mice (50 mg/kg/day i.p.) in vivo.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576400 D-I03 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear
£501.43 (exc VAT) per 25MG
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3576401 D-I03 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear
£124.24 (exc VAT) per 5MG
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